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新型儿茶酚取代头孢菌素GR69153的作用模式及其与tonB依赖性铁转运系统的相互作用。

Mode of action of GR69153, a novel catechol-substituted cephalosporin, and its interaction with the tonB-dependent iron transport system.

作者信息

Silley P, Griffiths J W, Monsey D, Harris A M

机构信息

Chemotherapy Department, Glaxo Group Research Limited, Greenford, United Kingdom.

出版信息

Antimicrob Agents Chemother. 1990 Sep;34(9):1806-8. doi: 10.1128/AAC.34.9.1806.

DOI:10.1128/AAC.34.9.1806
PMID:2285295
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC171932/
Abstract

GR69153 is a novel cephalosporin incorporating a catechol-substituted 7-aminothiazolyl-oxime. The antibiotic is actively transported into gram-negative cells via iron-regulated outer membrane proteins regulated by the tonB product. This transport enhances bactericidal activity most significantly at low concentrations, essentially removing the permeability barrier for antibiotic uptake.

摘要

GR69153是一种新型头孢菌素，其包含一个儿茶酚取代的7-氨基噻唑肟。该抗生素通过由tonB产物调控的铁调节外膜蛋白被主动转运至革兰氏阴性菌细胞内。这种转运在低浓度时最显著地增强杀菌活性，基本消除了抗生素摄取的通透性屏障。

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